Synthesis 2015; 47(19): 3067-3078
DOI: 10.1055/s-0034-1378845
paper
© Georg Thieme Verlag Stuttgart · New York

An Efficient Route to N-Monosubstituted Guanidino-Lactams

Autoren

  • Sara Tommasi

    a   Kosterlitz Centre for Therapeutics, Institute of Medical Sciences, University of Aberdeen, Foresterhill AB25 2ZD, Scotland, UK
  • Chiara Zanato

    a   Kosterlitz Centre for Therapeutics, Institute of Medical Sciences, University of Aberdeen, Foresterhill AB25 2ZD, Scotland, UK
  • Rey Carabeo

    b   Bacteriology Section, Programme in Microbiology, Institute of Medical Sciences, University of Aberdeen, Foresterhill AB25 2ZD, Scotland, UK
  • Arduino A. Mangoni

    c   Department of Clinical Pharmacology, School of Medicine, Flinders University and Flinders Medical Centre, Bedford Park, SA 5042, Australia
  • Sergio Dall’Angelo

    a   Kosterlitz Centre for Therapeutics, Institute of Medical Sciences, University of Aberdeen, Foresterhill AB25 2ZD, Scotland, UK
  • Matteo Zanda*

    a   Kosterlitz Centre for Therapeutics, Institute of Medical Sciences, University of Aberdeen, Foresterhill AB25 2ZD, Scotland, UK
    d   C.N.R.-I.C.R.M., via Mancinelli 7, 20131 Milano, Italy   eMail: m.zanda@abdn.ac.uk
Weitere Informationen

Publikationsverlauf

Received: 15. Februar 2015

Accepted after revision: 05. Juni 2015

Publikationsdatum:
25. Juni 2015 (online)


Graphical Abstract

Abstract

A small library of guanidino-lactams were synthesized in four steps and good overall yields by following the routes: preparation of guanylating agents, synthesis of protected guanidino-acids, cyclization to fully protected guanidino-lactams, and deprotection to the target compounds. The guanidino-lactams were assayed as antimicrobials on E. coli showing no significant antibiotic activity.